Target intelligence / Profile preview

Low-density lipoprotein (LDL) and other apolipoprotein B-containing (apoB) lipoprotein particle (LDL and apoB-containing lipoproteins)

Target
LDL and apoB-containing lipoproteins
Molecular classification
Other
01

Overview

Circulating low-density lipoprotein (LDL) and other apolipoprotein B (apoB)-containing particles, including very-low-density lipoprotein (VLDL) and intermediate-density lipoprotein (IDL), are macromolecular complexes that transport cholesterol and triglycerides through the bloodstream (NIH, 2023). Each of these atherogenic particles contains a single molecule of apolipoprotein B-100, which provides structural stability and serves as the primary ligand for the LDL receptor (LDLR) (UniProt, 2024). Elevated levels of these particles are a fundamental cause of atherosclerosis, as they can infiltrate the arterial wall and initiate the formation of lipid-rich plaques (PubMed, 2020). Pharmacological management of cardiovascular risk focuses on lowering the concentration of these particles using various therapeutic classes. Statins and PCSK9 inhibitors work by increasing the density of hepatic LDL receptors to enhance particle clearance, while agents like ezetimibe reduce the influx of cholesterol into the liver (StatPearls, 2023). More specialized therapies, such as lomitapide and mipomersen, directly inhibit the assembly or synthesis of the apoB-containing particles themselves (PubChem, 2024).

Other names
LDLApolipoprotein B-containing lipoproteinsApoB-lipoproteinsLow-density lipoproteinVery-low-density lipoproteinIntermediate-density lipoproteinBad cholesterolAtherogenic lipoproteins
02

Mechanism of action

Reduction of circulating levels through increased hepatic clearance via LDL receptor upregulation, inhibition of hepatic synthesis (MTP or APOB inhibition), or inhibition of intestinal cholesterol absorption (StatPearls, 2023).

03

Biological functions

Other
04

Disease associations

Cardiovascular diseaseOther
05

Safety considerations

Myopathy and rhabdomyolysisHepatotoxicityIncreased risk of new-onset type 2 diabetesInjection site reactionsHepatic steatosis (with MTP inhibitors)
06

Interacting drugs

Atorvastatin

11 more in the full profile.

07

Biomarkers

LDL-C (Low-density lipoprotein cholesterol)Apolipoprotein B (apoB)Non-HDL-CRemnant cholesterolLp(a)

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